The European research infrastructure for chemical biology and early drug discovery (EU-OPENSCREEN)

The European research infrastructure initiative EU-OPENSCREEN ¹ (www.eu-openscreen.eu) supports scientists to implement their early drug discovery projects on a collaborative basis. Through its more ca. 30 academic partner institutes across nine European countries, it offers complementary expertise and access to technology platforms for the development of novel chemical probes and early hit compounds for the life sciences community.

Scientists who successfully applied to implement their discovery projects with EU-OPENSCREEN transfer their assays to one of EU-OPENSCREEN screening partner sites. All partner sites jointly use a unique diversity compound collection containing ca. 100,000 commercial compounds and a growing collection of compounds that have been submitted by chemists from all over Europe. The partner sites have a track record of compound screening campaigns across a wide range of formats, including biochemical, cell-based, and model organism-based screens. Specialist screening sites complement larger high-capacity screening sites by offering specialised expertise and technologies that are not commonly available at the high-capacity screening facilities (e.g., BSL3 capacities). The primary screening data (including data of inactive compounds) are made available to the scientific community via its open-access European Chemical Biology Database (https://ecbd.eu/). Post-screening, EU-OPENSCREEN's medicinal chemistry partner sites support the hit-to-lead optimisation to improve the potency, selectivity, and in vitro/in vivo ADMET properties of the identified compounds. Confirmation of drug mechanism of action and target engagement studies are supported by our chemoproteomics sites and can be realised via close collaborations with structural biology partners in the INSTRUCT community

Compound repurposing is an important strategy for the identification of effective drugs. EU-OPENSCREEN designed a compound collection of 2,464 known bioactives with high target selectivity against 1,039 different targets. This bioactives collection contains 654 approved drugs and 368 highly selective probes from the public domain. In addition, various drug repurposing collections are available for drug repurposing studies at our partner sites, including the most comprehensive and up-to-date biologically annotated collections of FDA-approved compounds based on the Drug Repurposing Hub ² and ReFRAME ³ library.